Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs

Kim, Kyung Soo; Jin, Sung Giu; Mustapha, Omer; Abid, Sharjeel; Kim, Dong Wuk; Kim, Young Hun; Kim, Jong Oh; Yong, Chul Soon; Woo, Jong Soo; Choi, Han‐Gon

doi:10.1016/j.ijpharm.2015.05.059

Cited by 34 publications

(18 citation statements)

References 44 publications

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“…After oral administration, fenofibrate (prodrug) was biotransformed to fenofibric acid (active metabolite). In this study, the determination of its bioavailability was revealed by assay of its metabolite, because no fenofibrate was detectable in plasma following oral administration (Tang et al, 2009;Kim et al, 2015;Yousaf et al, 2015c;Yousaf et al, 2016). Formulations I and IV provided higher plasma concentrations of fenofibric acid than did the drug powder at all time points, with significant differences (P < 0.05) at 0.5-24 h and 2-24 h for formulations I and IV, respectively.…”

Section: Resultsmentioning

confidence: 99%

“…Then, the separated plasma samples were kept at À20 C until HPLC analysis. Sample preparation for HPLC analysis -Fenofibrate, a prodrug, is completely biotransformed to fenofibric acid, an active metabolite, by body esterases; therefore, the bioavailability assessment of fenofibrate is established by the measurement of fenofibric acid in plasma (Tang et al, 2009;Kim et al, 2015;Yousaf et al, 2015cYousaf et al, , 2016. Fenofibric acid was extracted from plasma by a liquid-liquid extraction technique.…”

Section: Pharmacokineticsmentioning

confidence: 99%

“…Then, their aqueous solubility, dissolution, physicochemical properties using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infra-red spectroscopy (FT-IR), and pharmacokinetics in rats were assessed relative to the drug powder. Here, fenofibrate was used as a model poorly watersoluble drug because it is classified as BCS Class II due to its insolubility in aqueous media and high lipophilicity (Tran et al, 2014;Kim et al, 2015;Yousaf et al, 2016). PVP has been used frequently as a carrier in the preparation of conventional solventevaporated microspheres (Dave et al, 2013;Oh et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

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Influence of polyvinylpyrrolidone quantity on the solubility, crystallinity and oral bioavailability of fenofibrate in solvent-evaporated microspheres

Yousaf

Kim

et al. 2016

Journal of Microencapsulation

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The objective of this study is to explore the influence of polyvinylpyrrolidone (PVP) quantity on the solubility, crystallinity and oral bioavailability of poorly water-soluble fenofibrate in solvent-evaporated microspheres. Numerous microspheres were prepared with fenofibrate, sodium lauryl sulphate (SLS) and PVP using the spray-drying technique. Their aqueous solubility, dissolution, physicochemical properties and pharmacokinetics in rats were assessed. The drug in the solvent-evaporated microspheres composed of fenofibrate, PVP and SLS at the weight ratio of 1:0.5:0.25 was not entirely changed to the amorphous form and partially in the microcrystalline state. However, the microspheres at the weight ratio of 1:4:0.25 provided the entire conversion to the amorphous form. The latter microspheres, with an improvement of about 115 000-fold in aqueous solubility and 5.6-fold improvement in oral bioavailability compared with the drug powder, gave higher aqueous solubility and oral bioavailability compared with the former. Thus, PVP quantity played an important role in these properties of fenofibrate in the solvent-evaporated microspheres.

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Section: Resultsmentioning

confidence: 99%

Section: Pharmacokineticsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Influence of polyvinylpyrrolidone quantity on the solubility, crystallinity and oral bioavailability of fenofibrate in solvent-evaporated microspheres

Yousaf

Kim

et al. 2016

Journal of Microencapsulation

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“…Each nanospherule formulation, equivalent to 15 mg of fenofibrate, was properly enclosed in a dialysis bag (Spectra/Por ® dialysis membrane, molecular weight cutoff: 3,500 Da; Spectrum Laboratories, Rancho Dominguez, CA, USA) and the loaded bag was placed in the basket. The basket was immersed in 500 mL of 2% (w/v) aqueous Tween 80 27,28 at 37°C±0.5°C. The rotation speed of the basket was set to 100 rpm.…”

Section: Dissolution Testmentioning

confidence: 99%

Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate

Yousaf

Mustapha

Kim

et al. 2016

IJN

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Purpose The purpose of the present research was to develop a novel electrosprayed nanospherule providing the most optimized aqueous solubility and oral bioavailability for poorly water-soluble fenofibrate. Methods Numerous fenofibrate-loaded electrosprayed nanospherules were prepared with polyvinylpyrrolidone (PVP) and Labrafil ® M 2125 as carriers using the electrospray technique, and the effect of the carriers on drug solubility and solvation was assessed. The solid state characterization of an optimized formulation was conducted by scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopic analyses. Oral bioavailability in rats was also evaluated for the formulation of an optimized nanospherule in comparison with free drug and a conventional fenofibrate-loaded solid dispersion. Results All of the electrosprayed nanospherule formulations had remarkably enhanced aqueous solubility and dissolution compared with free drug. Moreover, Labrafil M 2125, a surfactant, had a positive influence on the solubility and dissolution of the drug in the electrosprayed nanospherule. Increases were observed as the PVP/drug ratio increased to 4:1, but higher ratios gave no significant increases. In particular, an electrosprayed nanospherule composed of fenofibrate, PVP, and Labrafil M 2125 at the weight ratio of 1:4:0.5 resulted in a particle size of <200 nm with the drug present in the amorphous state. It demonstrated the highest solubility (32.51±2.41 μg/mL), an excellent dissolution (~85% in 10 minutes), and an oral bioavailability ~2.5-fold better than that of the free drug. It showed similar oral bioavailability compared to the conventional solid dispersion. Conclusion Electrosprayed nanospherules, which provide improved solubility and bioavailability, are promising drug delivery tools for oral administration of poorly water-soluble fenofibrate.

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“…The pellet is bioequivalent to the commercial product in beagle dogs. 14 Additionally, a mixture of FA and magnesium carbonate at a weight ratio of 2/1 can improve the solubility, dissolution, and oral bioavailability of FA. 9 No information about the in vitro-in vivo correlation (IVIVC) of this drug is available.…”

Section: Introductionmentioning

confidence: 99%

Comparative <i>In Vitro</i> and <i>In Vivo</i> Evaluation of Fenofibric Acid as an Antihyperlipidemic Drug

Windriyati¹,

Sumirtapura²,

Pamudji³

2020

tjps

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Amaç: Fenofibrik asit (FA) antihiperlipidemik bir ajandır ve 105 mg aktif madde içeren 840 mg ağırlığında bir tablet formülasyonu şeklinde ticari olarak temin edilebilir. Konvansiyonel formülasyona alternatif olarak inaktif madde miktarı daha az yeni bir formülasyon geliştirildi. Bu çalışmanın amacı, yüzey katı dispersiyonunun (SSD) ve konvansiyonel FA formülasyonlarının disolüsyonunu ve göreceli biyoyararlanımını ticari tabletlerindeki referans formülasyon ile karşılaştırmaktır. Bu tablet formülasyonları arasındaki in vitro-in vivo korelasyon da değerlendirildi. Gereç ve Yöntemler: Disolüsyon deneyleri fosfat tamponu pH 6,8 ve açlık durumu yapay bağırsak sıvısı içinde yapıldı. Disolüsyon profillerini karşılaştırmak için disolüsyon verimliliği ve ortalama disolüsyon süresi (MDT) kullanıldı. Dokuz sağlıklı gönüllü üzerinde gerçekleştirilen biyoyararlanım çalışması, tek doz, aç karna, randomize, çapraz bir tasarım kullanılarak gerçekleştirildi. In vivo performans, C max , T max , AUC 0-72 ve AUC 0-∞ farmakokinetik parametreleri kullanılarak karşılaştırıldı. MDT ve ortalama kalış süresi (MRT) kullanılarak doğrusal korelasyon modeli test edilmiştir. Bulgular: Sonuçlar, çözünme performanslarında önemli farklılıklar olduğunu, ancak SSD, geleneksel ve referans formülasyonlardan tahmin edilen ortalama C max , T max , AUC 0-72 veya AUC 0-∞ arasında önemli farklılıklar olmadığını gösterdi. Üç formülasyonun MRT ve MDT değerleri arasında zayıf bir korelasyon bulundu. Sonuç: SSD formülasyonu, polimerin varlığı ve SSD'nin fiziki yapısı nedeniyle ilacın ani disolüsyonuna yol açtı. Konvansiyonel formülasyon, hızlı salım dozaj formu gereksinimini karşılamasına rağmen disolüsyonu hızlı olmadı. Her iki formülasyon da referansın biyoeşdeğeri olarak değerlendirilebilir.

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Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs

Cited by 34 publications

References 44 publications

Influence of polyvinylpyrrolidone quantity on the solubility, crystallinity and oral bioavailability of fenofibrate in solvent-evaporated microspheres

Influence of polyvinylpyrrolidone quantity on the solubility, crystallinity and oral bioavailability of fenofibrate in solvent-evaporated microspheres

Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate

Comparative <i>In Vitro</i> and <i>In Vivo</i> Evaluation of Fenofibric Acid as an Antihyperlipidemic Drug

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